C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/253, 260/313
C07D 405/12 (2006.01) C07D 307/24 (2006.01) C07D 405/06 (2006.01) C07D 405/14 (2006.01)
Patent
CA 2028953
PROCESS FOR THE PREPARATION OF QUINAZOLINE DERIVATIVES Abstract The invention relates to a process for the preparation of quinazoline derivatives of the general Formula I (I) Image [wherein R1 and R2 may be the same or different and stand for hydrogen or lower alkyl or together form an ethylene (-CH2-CH2-) or trimethylene (-CH2-CH2- -CH2-) group; and n is the integer number 2 or 37 and pharmaceutically acceptable acid addition salts thereof, which comprises a) reacting an isothiourea derivative of the general Formula III -2- Image (III) [wherein R stands for lower alkyl or phenyl-lower alkyl, where the phenyl ring of the latter group may be optionally substituted by one or more lower alkyl group(s) and/or halogen atom(s)] with an amine of the general Formula IV, Image (IV) (wherein R1, R2 and n are as stated above) at a temperature between 150 °C and 280 °C; or b) cyclising a compound of the general Formula II Image (II) -3- (wherein R1, R2 and n are as stated above) optionally in the presence of a catalyst; and, if desired, converting a compound of the general Formula I thus obtained into a pharmaceutically acceptable acid addition salt thereof.
Csorgo Margit
Fekete Marton
Gorgenyi Frigyes
Pongo Laszlo
Reiter Jozsef
Egis Gyogyszergyar Rt.
G. Ronald Bell & Associates
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